Composition for inhalation therapy and methods for use

ABSTRACT

A composition for providing aromatherapy, and in particular, symptomatic relief of nasal and sinus congestion is provided in unit dosage format. The composition includes a penetrating aromatic vapor whose release from a preparation of warm water is augmented by an effervescent component which reacts in the warm water to promote release of the aromatic fragrance, or sustained over time by tableting or gelatin encapsulation. As the fragrance is inhaled, symptomatic relief is obtained. The composition of matter may be rendered ingestible, so that the warm water containing the composition is consumed following inhalation. In preferred embodiments, the release of the penetrating aromatic fragrance persists over time.

BACKGROUND OF THE INVENTION

1. Field of the Invention

This invention pertains to a composition which can be used to securerelief from congestion of the nasal passages as well as sinuscongestion, by inhalation of penetrating aromatic fragrances from a warmliquid. The invention also pertains to methods of obtaining such relief,as well as related benefits of inhalation therapy.

2. Background of the Technology

The actual background of inhalation therapy is quite old. A wide varietyof products have been used over the years to generate the release ofaromas that are pleasant, therapeutic or otherwise beneficial, toachieve relaxation, temporary relief from upper respiratory distress,and a variety of related conditions. As just one example, candles forwhat is generally regarded as “aroma therapy” are widely sold incommercial markets and in spas and other businesses offering cosmeticand therapeutic benefits, with various moods said to be induced by theselection of particular fragrances. By the same token, there are avariety of products on the market that rely, in whole or in part, on therelease of specific flavors and/or fragrances, to achieve theirbeneficial affects, in part or in whole. In addition to the candlesmentioned above, a number of products are available in oil form, whichgenerally comprises essence of the flavor or fragrance, combined with anoil that is either tolerable on the skin, ingestible, or otherwisecompatible for human use. A wide variety of aroma therapy oils are knownthat use, among other flavors and fragrances, peppermint, eucalyptus,spearmint, camphor and rosemary. A product marketed by “Origins” underthe name “Open For Business™” is intended to provide relief for nasalpassages, and is available in an oil form, that employs one or more ofmethanol, rosemary, lavender, eucalyptus, spearmint, pine, artemisia andcamphor as effective agents. Like candles, oil preparations presentpractical problems in use and application, are not easily used in a widevariety of locations, and are not dosage or user friendly, in that theyrequire the use of careful monitoring of the amount used, and may not beamenable to application in a wide variety of areas.

Other products that are available in liquid form include materialsintended to be added to bath water, such as Johnson's Soothing VaporBathe and Mentholatum Gentle Soothing Vapor Bath® as well as liquidsintended to be added to a vaporizer, generally available from Vicks,under such marks as “Vapo Steam®.” Other products that also requireaddition to a bath for effectiveness include a variety of bath salts,and a bath bomb, which is a molded effervescent bath ball. As with theoils, these products are not generally applicable for use, but requireprivacy. Further, their duration is short lived, and cannot be prolongedover time. In particular, an introduction to water, they immediatelydissolve or otherwise release the fragrance over a very short time span.

Other products include recognized therapeutic/pharmaceutical agents,such as cough suppressants, and decongestants (cough drops, e.g., Halls®mentho-lyptus) as well as analgesics, such as TheraFlu®, which appear inthe forms of lozenges or powders.

Finally, a variety of teas, which originally represent infusions ofvarious natural substances, but may contain extracts or preparation ofthe isolated flavors have been known for thousands of years, examplesincluding mint and peppermint-based teas.

All of these existing forms of therapy, which rely to a greater orlesser extent on the use of flavor and/or fragrances to bring relief ofsinus and nasal congestion, have one or more practical difficulties inuse. They are not generally susceptible to transportation and useanywhere. Many of them require careful measurement for dosing, andrequire preparation of a bath, a vaporizer, and the privacy associatedtherewith, for use. Many of these prior art compositions and techniquesalso release aroma over a very short duration—this is particularly ofpowders, liquids and teas, where the fragrance is released essentiallyimmediately, and is of short duration.

A variety of U.S. patents have issued directed to these types of priorart. These include U.S. Pat. Nos. 4,568,560; 5,041,421; 5,198,144;5,238,915; 5,382,567, 5,957,370; 5,980,880; 5,997,901; 6,180,092;6,244,265; 6,280,751; 6,289,967; 6,374,044; 6,413,476 and 6,447,816.None of these patents address a single dosage product provided in acompact form that is easily transported, and used without regard toneeds for privacy, generally anywhere, to provide for sustained releaseof penetrating aromatic fragrances that can relieve the symptomsassociated with congestion.

Another form of inhalation therapy is addressed in U.S. Pat. No.5,993,854, commonly assigned herewith. In this patent, the tablet isdesigned for introduction in a shower or other environment where it isnot immersed in water, but rather it is contacted with water, to providefor release of a volatile agent. The product requires the combination ofboth an effervescent agent and an exothermic agent, and of course if notsusceptible of use generally, in public areas.

Accordingly, it is an object of the art to provide a composition ofmatter that can be used to achieve at lease temporary relief of thesymptoms associated with congested nasal passages and sinuses by theinhalation of penetrating aromas, in a compact solid dosage form such asa tablet, gel or the like, which can be easily transported, and usedeasily, everywhere, without the existing requirements for privacy, time,etc. Ideally, such materials are designed to release the penetratingaromatic material over at least a limited period of time, so that somesustained release can be achieved.

SUMMARY OF THE INVENTION

The above objects, and other objects related to the provisions ofinhalation therapy materials, are met by combining one or more of afamily of penetrating aromatic materials with an effervescentcomposition, which, when mixed in warm water, effervesces to promoterelease of the penetrating aromatic material. The composition ispresented in dosage form, typically, in the form of a tablet, althoughcapsules and similar formats may be used.

The penetrating aromatic material, are not confined or uniformlycharacterized by any single given feature or characteristic, includingvapor pressure, volatility, molecular weight and the like. Penetratingaromatic materials that may be used in connection with this inventioninclude:

Penetrating Aromatic Materials

-   Aldehyde C-6, C-7, C-8, C-9, C-10, C-11 Geranyl Nitrile-   Allyl Caproate Ginger Oil-   iso Amyl Acetate Hydrotropic Aldehyde-   Amyl Butyrate Indole-   Armoise Oil (cedarleaf) Iso Bomyl Acetate-   Anethole Lavandin Abrialis-   Basil Oil Lavender Oil-   Benzaldehyde Methyl Cinnamate-   Cassia Oil Methyl Octine Carbonate-   Camphor Methyl Benzoate-   Carvone (l- or d-) Methyl Salicylate-   Cinnamic Alcohol Menthol-   Cinnamic Aldehyde Para Cresol-   Cis 3 Hexenol/al Peppermint Oil-   Citral Petitgrain Oil-   Citronellal Pine Oil (terpenes)-   Clove Oil Phenyl Acetaldehyde-   Cornmint Oil Rosemary Oil-   Ethyl Acetate Sage Oil-   Ethyl Butyrate Sage Oil Dalmation-   Ethyl Caproate Spearmint Oil-   Eucalyptol Styrallyl Acetate-   Eucalyptus Oil Tea Tree Oil-   Eugenol Turpentine-   Galbanum Oil Trans-2-cis-6 Nonadienal/ol-   Geramium Oil Triplal

The penetrating aromatic components may be anhydrous derivatives, otherpowders, or in liquid form. In particulate or powder form, the aromaticmaterials are formulated together with an effervescent component, whichis designed to react with release of effervescence upon introduction ofthe dosage form into warm water or other heated aqueous material.Although a wide variety of effervescent components are known, exemplaryeffervescent components include fumaric acid, sodium bicarbonate, sodiumcarbonate, as well as binders, lubricants and carriers, such aspolyethylene glycol (PEG) sorbitol and maltodextrin. A suitable tabletcan be prepared. As the dosage form of the claimed invention is intendedto be introduced into heated water or other aqueous solution, and therelease of penetrating aromatic agents is preferably prolonged overtime, the composition is formulated to dissolve/release relativelyslowly, rather than instantly. In a tablet form, this can be achieved byselection of appropriate binders and/or tablet processing conditions. Ina capsule, some of the penetrating aromatic materials may be entrainedin a slowly dissolving gel comprising the capsule wall. The inventionmay be further modified by the incorporation of colorants, fillers, andother inert materials.

DETAILED DESCRIPTION OF THE INVENTION

The invention begins with the appreciation of the importance of acompact, solid dosage form of product that is easily transported, andpre-measured for uniform dosing. The product permits the delivery ofhigh impact aromatic materials without the preparation of shower, bathor vaporizer, without exaggerated requirements for privacy, and providesfor a sustained release, where desired, of the penetrating aromaticmaterial. Ideally, accordingly, the solid dosage form is prepared in theform of a tablet, which provides a low cost, easily used format that theultimate consumer may simply unwrap and drop into warm water (generally,above about 100°-150° F.). The temperature of the water serves only toenhance both dissolution of the tablet and release of the penetratingaromatic material. In preferred embodiments, the tablet is prepared withbinders selected so as to retard dissolution of the tablet in the warmwater. Tableting conditions and formulations can also be selected toretard the rate of release. For instance, it is well known to tabletformulators that increasing the hardness of tablets, either bymechanical means (increased compression forces) or by chemical means(high strength binders) will slow their dissolution time. Alternativedosage forms are also easily employed to release the aromatic materialover an extended period of time. Thus, one dosage form within theinvention is a gel capsule. The fragrance oils of the claimed inventionmay be carried in a gelatin capsule that dissolves over time. Thefragrance can be either carried in a vehicle oil, which may be eithermineral or vegetable oil, or in the alternative, using conventionaltechnology, it may be micro encapsulated in an appropriate matrix thatis formulated within the outer gelatin capsule of the dosage form. Asthe capsule dissolves in warm water, the effervescent action componentis released, enhancing delivery of the penetrating aromatic material,which is released over time, as the gelatin dissolves. Conventionalgelatins such as natural gelatins manufactured from bovine hides and“vegetarian” gelatins made from polymers such as hydroxypropyl methylcellulose are known to those of skill in the art.

As discussed above, in one embodiment, the invention embraces the rapidrelease of penetrating vapors from the surface of the warm liquid inwhich the composition is placed. The effervescent component (reactantswhich combine, in the warm liquid, to release carbon dioxide) ensuresthat useful levels of penetrating aroma are released relatively quickly,nearly instantaneously. In an alternative embodiment, where the user iscontent to wait a short period of time (typically one to five minutes)to build up the level of vapor released, and the relief obtained, theeffervescent component is unnecessary. In this embodiment, thecomposition is prepared to provide sustained release (a substantiallyconstant level of vapor is released from the surface of the liquid overthe period of use). This can be achieved by preparing aneffervescent-free composition of sufficient density (tablets, caplets)so as to retard rapid dissolution and release of the entrainedoils/aromas. In general, a density of about 1.4 g/cc or higher isrequired. In the alternative, a gelatin encased capsule, or gelcap, canbe prepared, that is made from a slowly dissolving gelatin, with thearomatic materials contained within and/or as part of the gelatin wallof the capsule. A large variety of “softgels” are available for thisuse. Exemplary ones include those available from Cardinal Health ofSomerset, N.J. under the brand “Scherersols.” The period of release canbe up to 20-30 minutes or more.

Subsequent to the making of the invention claimed herein, the inventorcommunicated this invention to a company which subsequently, but lessthan one year prior to the filing date of this application withoutpermission, marketed the invention as “Vapor Shot”. While not prior artto this invention, Vapor Shot reflects one application of the technologydisclosed and claimed herein. Representative formulations are providedherewith. Sample Formulations (%/w/w) Effervescent Non-EffervescentMaterial Tablet Tablet Fumaric Acid 38.0 Sodium Bicarbonate 19.0 SodiumCarbonate 19.0 PEG-180 2.0 1.0 Sorbitol 14.0 Dextrates 88.0 SoyPolysaccharides 2.0 Sodium Benzoate 2.0 Maltodextrin 4.0 3.5 Silica 0.5Fragrance 3.5 3.5 Color As desired As desired TOTAL 100.0 100.0

As noted above, the single dosage formulation of the claimed inventionis designed to be added to hot water. As the penetrating aromaticmaterial is released, the container of hot water (cup, bowl or the like)is held in close proximity to the nose, and the penetrating aromaticmaterial being released inhaled by the user. Clearly, the product neednot be ingestible. Given the nature of the product, and the associationsof some of the aromatic oils with flavors familiar to a wide spectrum ofusers, however, it may be desirable to render the product ingestible aswell as suitable for inhalation of the penetrating vapors released.Under such conditions, care should be taken to formulate theeffervescent product with materials that are safe for ingestion, andsuitable flavorants may be added. For maximum performance, the productis first inhaled, and then, as the quantity of penetrating aromaticmaterial released is reduced, the product may then be ingested asdesired.

While the product may be formulated in capsule, caplets, tablet form andthe like, one exemplary form, for the treatment of sinus congestion andthe alleviation of symptoms associated therewith, is a single dosagetablet. The tablet is prepared using conventional tableting pressequipment and processes, compressing the dry ingredients set forthbelow. This representative embodiment releases the penetrating andsoothing vapors of mental and eucalyptus to provide immediate relieffrom the symptoms associated with sinus congestion. Component % w/wCitric Acid 40.000 Sodium Carbonate 20.000 Sodium Bicarbonate 20.000PEG-180 2.000 Silica 0.250 Maltodextrin 2.500 Sorbitol 13.710 Menthol0.500 Eucalyptus Oil 1.000 Blue 1 Lake 0.015 Yellow 5 Lake 0.025 TOTAL100.000

While the embodiments of this invention have been illustrated as usefulin the relief of sinus and nasal congestion, the invention is not solimited, and can generally be used wherever aromatherapies findapplication. Those of skill in the art will select from the list ofpenetrating aromatic components to compound formulations that offerrelief other than from, or in addition to, sinus and nasal congestionsymptoms. For example, many of the penetrating aromatic materials listedare purported to deliver ‘emotional’ benefits traditionally associatedwith aromatherapy. Such benefits include stress relief, refreshment,invigoration, stimulation, relaxation (and/or calming), and aid insleeping.

The invention described above is described both generically, and byreference to specific example. The examples are not intended to belimiting, and should not be so construed, unless specifically soindicated in the claims. The invention relies on a variety of techniquesknown to those of skill in the art, that are not repeated in detailherein, including preparation of effervescent bases, tabletingprocesses, the formation of capsules and micro encapsulated particles,the preparation of ingestibles and the like. Those of skill in the artwill be aware of sources of information for such materials andprocesses, including various formulas and handbooks.

1. A composition of matter free of exothermic reactants, comprising: apenetrating aromatic fragrance selected from the group consisting of:Aldehyde C-6, C-7, C-8, C-9, C-10, C-11, Allyl Caproate, Iso AmylAcetate, Amyl Butyrate, Armoise Oil (Cedarleaf), Anethole, Basil Oil,Benzaldehyde, Cassia Oil Camphor, Carvone (l- or d-), Cinnamic Alcohol,Cinnamic Aldehyde, Cis 3 Hexenol/al, Citral, citronellal, clove oil,cornmint oil, ethyl acetate, ethyl butyrate, ethyl caproate, Eucalyptol,Eucalyptus Oil, Eugenol, Galbanum Oil Germium Oil, Geranyl Nitrile,Ginger Oil, hydrotropic aldehyde, indole, iso bomyl acetate, lavandinabrialis, lavender oil, Methyl cinnamate, methyl octine carbonate,methyl benzoate, methyl salicylate, Menthol, Para Cresol, PeppermintOil, Petitgrain Oil, Pine Oil (Terpenes), Phenyl Acetaldehyde, RosemaryOil, Sage Oil, Sage Oil Dalmation, Spearmint Oil, Styrallyl Acetate, TeaTree Oil, Turpentine, Trans-2-cis-6 Nonadienal/ol, and Triplal; whereinsaid composition further comprises an effervescent component which, whensolubilized in a warm aqueous liquid, effervesces, to improve release ofsaid penetrating aromatic fragrance from a surface of said liquid,whereby, on introduction of said composition of matter, which is insingle dosage form, into said liquid, said effervescing componenteffervesces, and said penetrating aromatic fragrance is released fromsaid warm liquid in a fashion sustained over the period of use so as toprovide aromatherapy to an individual in need thereof inhaling saidpenetrating aromatic fragrance.
 2. The composition of matter of claim 1,wherein said composition is in the form of a tablet, and furthercomprises a binder component, which retards dissolution and sustainsrelease of said penetrating aromatic fragrances.
 3. The composition ofclaim 1, wherein said single dosage form is a tablet, which has beentableted under conditions which retard release of said penetratingaromatic fragrance over the period of use.
 4. The composition of claim1, wherein said composition is in the form of a capsule which comprisesan exterior wall comprised of gelatin, which dissolves in said warmliquid over time.
 5. The composition of matter of claim 4, wherein saidgelatin wall further comprises at least one said penetrating aromaticfragrance, such that said at least one penetrating aromatic fragrance isreleased over the period of time said gelatin dissolves.
 6. A method ofproviding aromatherapy to a human individual in need of same, comprisingplacing the single dosage formulation of claim 1 in a container ofliquid comprising water of at least 100° F. allowing said composition tobe solubilized in said water, and allowing said patient to inhale saidpenetrating aromatic fragrance released from said water.
 7. The methodof claim 6, wherein said composition in said warm water is ingestible,and subsequent to said inhalation, said patient ingests saidcomposition.
 8. The method of claim 6, wherein said process providessymptomatic relief of sinus congestion, nasal congestion or respiratorydistress in said individual.
 9. The method of claim 6, wherein saidprocess provides at least one benefit selected from the group consistingof stress relief, refreshment, invigoration, stimulation, relaxation,calming and aid in sleeping to the user.
 10. A composition of matterfree of exothermic and effervescent reactants, comprising: a penetratingaromatic fragrance selected from the group consisting of: Aldehyde C-6,C-7, C-8, C-9, C-10, C-11, Allyl Caproate, iso Amyl Acetate, AmylButyrate, Armoise Oil (cedarleaf), Anethole, Basil Oil, Benzaldehyde,Cassia Oil Camphor, Carvone (l- or d-), Cinnamic Alcohol, CinnamicAldehyde, Cis 3 Hexenol/al, Citral, Citronellal, Clove Oil, CornmintOil, Ethyl Acetate, Ethyl Butyrate, Ethyl Caproate, Eucalyptol,Eucalyptus Oil, Eugenol, Galbanum Oil Germium Oil, Geranyl Nitrile,Ginger Oil, Hydrotropic Aldehyde, Indole, Iso Bomyl Acetate, LavandinAbrialis, Lavender Oil, Methyl Cinnamate, Methyl Octine Carbonate,Methyl Benzoate, Methyl Salicylate, Menthol, Para Cresol, PeppermintOil, Petitgrain Oil, Pine Oil (terpenes), Phenyl Acetaldehyde, RosemaryOil, Sage Oil, Sage Oil Dalmation, Spearmint Oil, Styrallyl Acetate, TeaTree Oil, Turpentine, Trans-2-cis-6 Nonadienal/ol, and Triplal; whereinsaid composition is in a single dosage formulation and further comprisesa binder, and is in the form of either (1) a compressed material havinga density in excess of 1.4 g/cc or (2) a gelatin encased capsule, whichgelatin resists rapid dissolution, such composition thereby providingsustained release of said penetrating aromatic fragrance from thesurface a warm aqueous liquid in which it is placed.
 11. A method ofproviding aromatherapy to a human individual in need of same, comprisingplacing the single dosage formulation of claim 10 in a container ofliquid comprising water of at least 100° F., allowing said compositionto be solubilized in said water, and allowing said patient to inhalesaid penetrating aromatic fragrance released from said water over aperiod of sustained release of said penetrating aromatic fragrance. 12.The method of claim 11, wherein said composition in said warm water isingestible, and subsequent to said inhalation, said patient ingests saidcomposition.
 13. The method of claim 11, wherein said process providessymptomatic relief of sinus congestion, nasal congestion or respiratorydistress in said individual.
 14. The method of claim 11, wherein saidprocess provides at least one benefit selected from the group consistingof stress relief, refreshment, invigoration, stimulation, relaxation,calming and aid in sleeping to the user.